Miscellaneous Derivatives of 8-Hydroxy-Quinoline**Scientific Section, A. Ph. A., Portland meeting, 1935.

1936 ◽  
Vol 25 (6) ◽  
pp. 501-504
Author(s):  
E. Moness ◽  
W.G. Christiansen
1975 ◽  
Vol 30 (9-10) ◽  
pp. 751-754 ◽  
Author(s):  
O. P. Pachauri ◽  
J. P. Tandon

Studies of the interaction between 1:1 Th(IV)-DTPA chelate (where DTPA = diethylenetriaminepentaacetic acid) with certain bidentate ligands, such as salicylic acid (SA), 5-sulphosalicylic acid (SSA) and 8-hydroxy quinoline-5-sulphonic acid (HQSA) have been carried out potentiometrically. The nature of the titration curves indicates that the bidentate ligand is added stepwise to the initially formed metal diethylenetriaminepentaacetate. The formation constants (log KMAB) of the resulting 1:1:1 mixed ligand derivatives have been determined at 30 ± 1 °C and μ = 0.1 (KNO3). The order of stability in terms of the secondary ligand has been found to be SA > SSA > HQSA.


Author(s):  
Bilquees Bano ◽  
Kanwal ◽  
Khalid Mohammed Khan ◽  
Almas Jabeen ◽  
Aisha Faheem ◽  
...  

Background:: Quinolines are important class of heterocyclic compounds possessing wide range of biological activities. Previously, we had identified Schiff bases of quinoline as potential anti-inflammatory agents, thus the current work is the continuation of our previous study. Objective:: In the current study 3-, 5-, and 8-sulfonamide and 8-sulfonate derivatives of quinoline (1-50) were synthesized and their antiinflammatory potential was evaluated. These synthetic analogs were evaluated for their anti-inflammatory activity via ROS (Reactive oxygen species) inhibitory effect produced from phagocytes from human whole blood. Methods:: The sulfonamide and sulfonate derivatives of quinoline were synthesized via treating 5-, 3-, 8-amino, and 8-hydroxy quinoline with different substituted sulfonyl chlorides in pyridine. The synthetic molecules were characterized using various spectroscopic techniques and screened for their anti-inflammatory potential. Results and Discussion:: Among the synthetic derivatives 1-50, six compounds showed good to moderate anti-inflammatory activity. Compounds 47 (IC50 = 2.9 ± 0.5 μg/mL), 36 (IC50 = 3.2 ± 0.2 μg/mL), and 24 (IC50 = 6.7 ± 0.3 μg/mL) exhibited enhanced activity as compared to the standard ibuprofen (IC50 = 11.2 ± 1.9 μg/mL). Compounds 20 (IC50 = 25.5 ± 0.7 μg/mL), 50 (IC50 = 42.9 ± 5.6 μg/mL), and 8 (IC50 = 53.9 ± 3.1 μg/mL) were moderately active, however, rest of the compounds were found to be inactive. Conclusion:: The sulfonamide and sulfonate derivatives of quinoline were found to have promising anti-inflammatory activity. Further studies on the modification of these molecules may leads to the discovery of new and potential anti-inflammatory agents.


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